Hewson G, Hill R G, Hughes J, Leighton G E, Turner W D
Parke-Davis Research Unit, Addenbrookes Hospital Site, Cambridge, U.K.
Neuropharmacology. 1987 Nov;26(11):1581-4. doi: 10.1016/0028-3908(87)90004-9.
The effects of the selective kappa opioid receptor agonists PD117302 [(+/-)trans-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl-]benzo-[b]- thiophene-4-acetamide] and U50488 (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide) were investigated on food intake in non-deprived rats over a 24 hr period following subcutaneous administration. At doses of 2.5 mg/kg and 5 mg/kg, both PD117302 and U50488 initially increased food intake. Between 6-24 hr, however, PD117302 (2.5-10 mg/kg) and U50488 (2.5 mg/kg and 5 mg/kg) caused a reduction in food intake. The largest doses of PD117302 and U50488 also reduced total 24 hr food intake. The reduction in food intake produced by PD117302 (5 mg/kg) was selective, since the intake of water was not affected. It is concluded that the kappa agonists PD117302 and U50488 produce a biphasic effect on 24 hr food intake, with an initial hyperphagia followed by a decrease in food intake.
研究了选择性κ阿片受体激动剂PD117302[（±）反式-N-甲基-N-[2-（1-吡咯烷基）-环己基-]苯并[b]-噻吩-4-乙酰胺]和U50488（反式-3,4-二氯-N-甲基-N-[2-（1-吡咯烷基）-环己基]-苯乙酰胺）对未禁食大鼠皮下注射后24小时内食物摄入量的影响。在2.5毫克/千克和5毫克/千克的剂量下，PD117302和U50488最初均增加了食物摄入量。然而，在6至24小时之间，PD117302（2.5至10毫克/千克）和U50488（2.5毫克/千克和5毫克/千克）导致食物摄入量减少。PD117302和U50488的最大剂量也减少了24小时的总食物摄入量。PD117302（5毫克/千克）引起的食物摄入量减少具有选择性，因为水的摄入量未受影响。得出的结论是，κ激动剂PD117302和U50488对24小时食物摄入量产生双相作用，最初是食欲亢进，随后是食物摄入量减少。
